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Dasotraline for ADHD


Dasotraline for ADHD

Dasotraline [(1R,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetra-hydronaphthalene-1-amine] is a dopamine and noradrenaline reuptake inhibitor with weak serotonin reuptake inhibition:1

  • DAT: IC50 = 3 nM
  • NET: IC50 = 4 nM
  • SERT: IC50 = 15 nM

Tetrodotoxin blocks neuronal firing and abolished the ability of dasotraline to increase synaptic monoamine concentrations, demonstrating that dasotraline is a reuptake inhibitor and not a monoamine releaser.1

Dasotraline has been tested for use in ADHD.23 RCTs showed an effect size of up to 0.484
Sunuvion is said to have discontinued the development of dasotraline in the meantime 54

Oral dasotraline is slowly absorbed in humans, with a tmax of 10-12 hours and a very long terminal elimination half-life of 47-77 hours.1 Dasotraline may have a sustained treatment benefit in ADHD due to its stable plasma concentration over 24 hours when administered once daily with a low potential for abuse.6 Dasotraline thus differs significantly from the rapid, large and short-lasting increase in dopamine efflux of d-amphetamine and MPH.

In a placebo-controlled double-blind study, a single daily dose of 8 mg dasotraline (but not 4 mg dasotraline) showed a significant improvement in ADHD-HI symptoms (ADHD-HI Rating Scale) and CGI-S scores after 4 weeks compared to placebo.7

At 4 mg, a good 10 % of the test subjects terminated the study prematurely, at 8 mg just under 28 %. This appears to be quite high.
The high insomnia could result from the long half-life of 47 hours, which on the other hand would allow a daily single dose that leads to a constant plasma level after 10 days of intake.89
On the other hand, insomnia was not a predictor for dropping out of the study.

Another 6-week RCT with 342 children aged 6-12 years found a significantly better improvement in ADHD symptoms at 4 mg/day than placebo with an effect size of 0.48. 2 mg/day showed no improvement10
The discontinuation rates due to adverse events were 12.2 % (4 mg/day), 6.3 % (2 mg/day) and 1.7 % (placebo).

Side effects in the studies were predominant (compared to placebo):

  • Sleep problems
    • These are likely to result from the long half-life
  • Dry mouth
  • Nausea
  • Postural orthostatic tachycardia syndrome (5.4 % vs. 0 %)
  • Perceptual disorders (5.4 % vs. 0 %)
  • Reduced appetite (10.7 % vs. 3.6 %)
  • Weight loss
  • Irritability (5.4 % vs. 3.6 %)
  • Headaches (10.7 % vs. 8.9 %)
  • Affect lability (8.9 % vs. 7.1 %)

A study on adults with 6 mg/day found only partially significant improvements in ADHD symptoms compared to placebo, but a trend towards improvement. This was due to a surprisingly large improvement in the placebo group 1112

There were no serious side effects or clinically relevant changes in blood pressure or heart rate.

  1. Heal DJ, Smith SL (2022): Prospects for new drugs to treat binge-eating disorder: Insights from psychopathology and neuropharmacology. J Psychopharmacol. 2022 Jun;36(6):680-703. doi: 10.1177/02698811211032475. PMID: 34318734; PMCID: PMC9150143. REVIEW

  2. Wigal, Hopkins, Koblan, Childress, Kent, Tsai, Hsu, Loebel, Goldman (2019): Efficacy and Safety of Dasotraline in Children With ADHD: A Laboratory Classroom Study. J Atten Disord. 2019 Aug 2:1087054719864644. doi: 10.1177/1087054719864644.

  3. Roll, Hahn (2016): Neue medikamentöse Behandlungsansätze. DNP – Der Neurologe und Psychiater. March 2016, Volume 17, Issue 3, pp 23–24

  4. Cortese S, McGinn K, Højlund M, Apter A, Arango C, Baeza I, Banaschewski T, Buitelaar J, Castro-Fornieles J, Coghill D, Cohen D, Grünblatt E, Hoekstra PJ, James A, Jeppesen P, Nagy P, Pagsberg AK, Parellada M, Persico AM, Purper-Ouakil D, Roessner V, Santosh P, Simonoff E, Stevanovic D, Stringaris A, Vitiello B, Walitza S, Weizman A, Wohlfarth T, Wong ICK, Zalsman G, Zuddas A, Moreno C, Solmi M, Correll CU (2023): The future of child and adolescent clinical psychopharmacology: A systematic review of phase 2, 3, or 4 randomized controlled trials of pharmacologic agents without regulatory approval or for unapproved indications. Neurosci Biobehav Rev. 2023 Jun;149:105149. doi: 10.1016/j.neubiorev.2023.105149. PMID: 37001575.

  5. Nazarova VA, Sokolov AV, Chubarev VN, Tarasov VV, Schiöth HB (2022): Treatment of ADHD: Drugs, psychological therapies, devices, complementary and alternative methods as well as the trends in clinical trials. Front Pharmacol. 2022 Nov 17;13:1066988. doi: 10.3389/fphar.2022.1066988. PMID: 36467081; PMCID: PMC9713849. REVIEW

  6. Vandana, Arnold (2019): Dasotraline in ADHD: novel or me too drug? Expert Rev Neurother. 2019 Apr;19(4):311-315. doi: 10.1080/14737175.2019.1593826. PMID: 30871381.

  7. Koblan, Hopkins, Sarma, Jin, Goldman, Kollins, Loebel (2015): Dasotraline for the Treatment of Attention-Deficit/Hyperactivity Disorder: A Randomized, Double-Blind, Placebo-Controlled, Proof-of-Concept Trial in Adults. Neuropsychopharmacology. 2015 Nov;40(12):2745-52. doi: 10.1038/npp.2015.124. PMID: 25948101; PMCID: PMC4864650. n = 331

  8. Hopkins, Sunkaraneni, Skende, Hing, Passarell, Loebel, Koblan (2016): Pharmacokinetics and Exposure-Response Relationships of Dasotraline in the Treatment of Attention-Deficit/Hyperactivity Disorder in Adults. Clin Drug Investig. 2016 Feb;36(2):137-46. doi: 10.1007/s40261-015-0358-7. PMID: 26597180; PMCID: PMC4740560.

  9. Roll, Hahn (2016): Neue Studien zu ADHS im Erwachsenenalter. DNP – Der Neurologe & Psychiater > Ausgabe 6/2018

  10. Findling, Adler, Spencer, Goldman, Hopkins, Koblan, Kent, Hsu J, Loebel (2019): Dasotraline in Children with Attention-Deficit/Hyperactivity Disorder: A Six-Week, Placebo-Controlled, Fixed-Dose Trial. J Child Adolesc Psychopharmacol. 2019 Mar;29(2):80-89. doi: 10.1089/cap.2018.0083. PMID: 30694697.

  11. Adler, Goldman, Hopkins, Koblan, Kent, Hsu J, Loebel (2021): Dasotraline in adults with attention deficit hyperactivity disorder: a placebo-controlled, fixed-dose trial. Int Clin Psychopharmacol. 2021 May 1;36(3):117-125. doi: 10.1097/YIC.0000000000000333. PMID: 33724251.

  12. Nageye, Cortese (2019): Beyond stimulants: a systematic review of randomised controlled trials assessing novel compounds for ADHD. Expert Rev Neurother. 2019 Jul;19(7):707-717. doi: 10.1080/14737175.2019.1628640. PMID: 31167583.)